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Alprazolam

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| bgcolor="#ffffff" align="center" colspan="2" | alprazolam chemical structure
Alprazolam |- | align="center" colspan="2" | IUPAC name |- align="center" style="border-bottom: 3px solid gray" | CAS number
28981-97-7 | ATC code
N05BA12 |- | bgcolor="#eeeeee" | Chemical formula | bgcolor="#ddeeff" | C17H13ClN4 |- | bgcolor="#eeeeee" | Molecular weight | bgcolor="#ddeeff" | 308.8 |- | bgcolor="#eeeeee" | Bioavailability | bgcolor="#ddeeff" | 80-90% |- | bgcolor="#eeeeee" | Metabolism | bgcolor="#ddeeff" | Liver |- | bgcolor="#eeeeee" | Elimination half life | bgcolor="#ddeeff" | 6-27 hours (11 hour avg.) |- | bgcolor="#eeeeee" | Excretion | bgcolor="#ddeeff" | Urine |- | bgcolor="#eeeeee" | Pregnancy category | bgcolor="#ddeeff" | D |- | bgcolor="#eeeeee" | Legal status | bgcolor="#ddeeff" | USA DEA Schedule IV |- | bgcolor="#eeeeee" | Route of administration | bgcolor="#ddeeff" | Oral |-

|- |Indicated for:
  • Anxiety
  • Panic attacks
Abuse:
  • Benzodiazepines are widely used for non-medical (i.e., recreational) purposes, and have occasionally been used as "date-rape" drugs
|- |Contraindications:
|- |Side effects:

Severe:

  • jaundice (rare)

Atypical sensations:

  • ?

Cardiovascular:

Ear, nose, and throat:

  • Nasal congestion

Endocrinal:

Eye:

  • Blurred vision
  • Difficulty in depth perception

Gastrointestinal:

Hematological:

  • Blood dyscrasias

Musculoskeletal:

  • Tremor

Central Nervous System:

  • Drowsiness
  • Headache
  • Dizziness
  • Insomnia
  • Paradoxical reactions including nervousness, agitation, rage, increased anxiety, insomnia, muscle spasms and rigidity (stop treatment immediately)
  • Sleep apnea syndrome

Psychiatric:

Respiratory:

  • Respiratory depression (use lower doses in the chronically ill or debilitated, those with pulmonary disease and the elderly)

Skin:

Urogenital and reproductive:

Miscellaneous:

  • ?

|} Alprazolam is a short-acting benzodiazepine used to treat anxiety disorders. It is generally sold in generic form (i.e., alprazolam) in the United States (to cut down on costs for insurance companies) and also under many other brand names, depending on the country:

  • Xanax® - United States, Australia, United Kingdom
  • Xanax XR® - (an extended release formulation) United States
  • Apo-Alpraz® - Canada (also made by other companies under different names)
  • Xanor® - Finland, Philippines, South Africa, Sweden
  • Kalma® - Australia, New Zealand
  • Ralozam® - Australia, New Zealand
  • Zamhexal® - Australia
  • Alplax® - Argentina
  • Alviz® - Indonesia
  • Alzolam® - India, Malaysia
  • Alprax® - India
  • Tranax® - India
  • Restyl® - Bahrain, Cyprus, Egypt, Iran, Iraq, Jordan, Kuwait, Lebanon, Libya, Oman, Qatar, Republic of Yemen, Saudi Arabia, Syria, United Arab Emirates
  • Tranquinal® - Ecuador, Peru
  • Trankimazin® - Spain
  • Tafil® - Costa Rica, Denmark, El Salvador, Germany, Guatemala, Honduras, Mexico, Nicaragua, Panama, Venezuela
  • Tafil AP® - (an extended release formulation) Mexico
  • Constan® - Japan
  • Solanax® - Japan
  • Zolarem® - Bahrain, Benin, Burkina-Faso, Cyprus, Egypt, Ethiopia, Gambia, Ghana, Guinea, Iran, Iraq, Israel, Ivory Coast, Jordan, Kenya, Kuwait, Lebanon, Liberia, Libya, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Oman, Qatar, Republic of Yemen, Saudi Arabia, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Syria, Tanzania, Tunia, Uganda, United Arab Emirates, Zambia, Zimbabwe
  • Zoldac® - Benin, Burkina-Faso, Ethiopia, Gambia, Ghana, Guinea, India, Ivory Coast, Kenya, Liberia, Malawi, Mali, Mauritania, Mauritius, Morocco, Niger, Nigeria, Senegal, Seychelles, Sierra-Leone, South Africa, Sudan, Tanzania, Tunia, Uganda, Zambia, Zimbabwe
  • Calmax® - Ireland

Alprazolam has a calming effect, with the most common side effects being drowsiness, clumsiness, and to a lesser extent, fatigue, and headache. It can also have more adverse effects, such as blurred vision, slurred speech or dysarthria, and changes in personality. It may be habit forming and users often develop a tolerance to its initial effects, although its anxiolytic efficacy remains intact. Physical and/or psychological dependence may develop after several weeks of alprazolam treatment. There is now a general consensus among many psychiatrists that alprazolam (a so-called 'high-potency' benzodiazepine) poses a particularly high risk for abuse and dependence. Withdrawal after long-term use should be done slowly over a period of weeks to avoid serious withdrawal symptoms such as agitation, rebound anxiety, muscle cramps and possible seizures. Some patients may benefit from a more gradual dosage reduction and/or discontinuation and substitution with diazepam.

Indications

File:Alprazolam2mgresize.jpg
alprazolam 2mg tablet bottle

The main medical indications are as follows:

1. Treatment of panic disorder (with or without agoraphobia). Alprazolam is very effective in preventing panic attacks. However, despite its efficacy, many psychiatrists are reluctant to use alprazolam for this condition because of the possibility of dependence and interdose anxiety due to its short-acting nature. An extended-release formulation of alprazolam known as Xanax XR® was introduced in 2001 and is often preferred.

2. As needed (PRN) therapy of panic attacks, 4 to 6 doses per month are the acceptable limit. If dependence seems to develop and/or the limit is exceeded therapy may be reconsidered and/or stopped.

3. Initial therapy together with selective serotonin reuptake inhibitors such as paroxetine, sertraline, or fluoxetine to alleviate initial SSRI-induced anxiety while waiting for the agent to begin working. Clinical experience has shown, however, that SSRIs may actually provoke panic attacks in otherwise healthy individuals and cause sexual dysfunction. In these cases, a tricyclic antidepressant may be used. Buspirone may also be useful in conjunction with alprazolam in cases of generalized anxiety disorder.

4. Long-term treatment of severe generalized anxiety disorders if other therapies either do not work or are contraindicated. Duration of therapy in this case is often four months or longer. The indication must be cautiously made by a specialized psychiatrist taking into account both the individual suffering, quality of life, loss in social performance and the risk of dependence.

5. The drug may be used by specialists to treat severe cases of Borderline Personality Disorder. Some studies have shown positive results.

Narcotic regulations

In the United States, alprazolam is a prescription drug and is assigned to Schedule IV of the Controlled Substances Act by the Drug Enforcement Administration. Internationally, alprazolam is included under the United Nations Convention on Psychotropic Substances[1].

Mechanism of action

Alprazolam is a triazolobenzodiazepine, that is, a benzodiazepine with a triazolo-ring attached to its structure. Alprazolam binds to the GABAA subtype of the GABA receptor, increasing inhibitory effects of GABA within the central nervous system. The binding site for benzodiazepines is distinct from the binding site for GABA on the GABA receptor.

Unlike other benzodiazepines, alprazolam may also have some antidepressant activity, although clinical evidence of this is lacking.

Pharmacokinetics

The mechanism of action is not fully understood; However, Alprazolam is readily absorbed from the gastrointestinal tract. The peak plasma concentration is achieved in 1-2 hours. Most of the drug is bound to plasma protein, mainly albumin. Alprazolam is hydroxylated in the liver to α-hydroxyalprazolam, which is also active. This and other metabolites are later excreted in urine as glucuronides. Some of the alprazolam is also excreted in unchanged form.

Recreational use

alprazolam 2mg tablets

Alprazolam, like other benzodiazepines, has the potential for abuse, especially in addiction-prone individuals. It is not manufactured illegally, but is sometimes diverted to the black market. Nasal (by snorting of ground tablets) administration sometimes occurs, though it is no more potent than when taken orally and often severely irritates the nasal passages. The state of relaxation, anxiolysis, disinhibition and euphoria induced by benzodiazepines is the main reason for their illicit use. It is sometimes used adjunctively with other recreational drugs to relieve the panic or distress of dysphoric reactions to psychedelics such as LSD and also to promote sleep (hypnosis) in the "come-down" period following use of recreational drugs with stimulant or insomniac properties (such as LSD, cocaine, amphetamines, and MDMA). It is also often used in conjuction with marijuana for an even more relaxing effect.

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